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Active ingredients
Dorzolamide
Release form
Drops
Composition
1 ml contains dorzolamide hydrochloride 22.26 mg, which corresponds to the content of dorzolamide 20 mg. Excipients: mannitol - 23 mg, gietelloza - 4.75 mg, sodium citrate - 2.94 mg, benzalkonium chloride - 0.075 mg, sodium hydroxide - for pH 5.5-5.8 correction, water d / and - up to 1 ml.
Pharmacological effect
The antiglaucoma action of Trusopt is achieved by inhibiting dorzolamide, the main component of the preparation of carbonic anhydrase II. By slowing down the synthesis of carbonic anhydrase, the drug reduces the production of intraocular fluid by the ciliary body. Reducing the amount of moisture in the chambers reduces the pressure inside the eye
Pharmacokinetics
When applied topically, dorzolamide penetrates the systemic circulation. With prolonged use, dorzolamide accumulates in erythrocytes as a result of selective binding to type II carbonic anhydrase, maintaining extremely low concentrations of free drug in plasma. As a result of the metabolism of dorzolamide, a single N-desethyl metabolite is formed, which less clearly blocks type II carbonic anhydrase compared to the starting material, but at the same time inhibits type I carbonic anhydrase (less active isoenzyme). The metabolite also accumulates in erythrocytes, where it binds mainly to type I carbonic anhydrase. About 33% of dorzolamide is bound to plasma proteins. Dorzolamide is excreted in the urine unchanged and as a metabolite. After stopping the use of the drug, dorzolamide is non-linearly washed out of red blood cells, which first leads to a rapid decrease in its concentration, and then elimination slows down. T1 / 2 is about 4 months. When receiving dorzolamide inside, in order to simulate the maximum systemic effects during its local application, an equilibrium state was achieved after 13 weeks. In addition, no free drug or its metabolites were actually detected in the plasma. Inhibition of erythrocyte carbonic anhydrase was insufficient to achieve a pharmacological effect on kidney function and respiration. Similar pharmacokinetic results were observed with long-term topical application of dorzolamide hydrochloride.However, in some elderly patients with renal insufficiency (creatinine clearance 30–60 ml / min), higher concentrations of the metabolite in erythrocytes were detected, but this did not have clinical significance.
Indications
Adults: ophthalmic hypertension; primary open-angle glaucoma; pseudoexfoliative glaucoma; secondary glaucoma (without anterior chamber angle block). Children: for treatment of glaucoma in children older than 1 week in monotherapy or as an adjunct to treatment with beta-adrenergic blockers
Contraindications
Chronic renal failure; - pregnancy; - lactation period (breastfeeding); - age less than 1 week; - hypersensitivity to the components of the drug. With caution The use of Trusopt has not been studied in patients with severe liver failure, and, consequently, to use the drug in this patient categories should be treated with caution
Precautionary measures
Use in patients who wear contact lensesPatients who wear contact lenses should consult a physician before using Trusopt. Trusopt contains benzalkonium chloride preservative, which can be adsorbed by contact lenses. Before using the drug lenses must be removed, do not wear lenses earlier than 15 minutes after instillation of the drug. Use in elderly patients In the studies performed, the efficacy and safety of Trusopt were the same in elderly and young patients. Use in patients with severe renal and hepatic insufficiency Patients who have been diagnosed or have had any liver or kidney disease, should inform your doctor. Effects on ability to drive and work with equipmentSome possible side effects of Trusopt may impair the ability to drive vehicles and work with equipment
Use during pregnancy and lactation
Contraindicated
Dosage and administration
When using Trusopt, the usual dose is 1 drop to the affected eye (or both eyes) in the morning, in the afternoon and in the evening. If you replace any antiglaucoma drug with Trusopt, you should start treatment with Trusopt from the next day after canceling the previous drug. Trusopt with other eye drops should be instilled at least 10 minutes apart. The rules for using the drug1.Before using the drug for the first time, make sure that the protective strip on the outside of the vial is intact. For unopened vials, there may be a gap between the bottle and the cap.2. Remove the protective strip in order to open the cap.3. To open the bottle, you must unscrew the cap, turning it in the direction of the directional arrows on the top surface of the cap. Do not pull the cap up in the direction from the bottle. Tilt the head back and slightly pull the lower eyelid down to create a space between the eyelid and the eye. Flip the bottle, with a thumb or index finger, lightly press in a place marked on the bottle so that one drop falls into the eye. Do not touch the surface of the eye or eyelid with the tip of the bottle. If used improperly, ophthalmic preparations can be infected by common bacteria that cause eye diseases. Serious damage to the eye and subsequent loss of vision may develop due to the use of infected ophthalmic preparations. If you suspect that the drug may be contaminated or if an eye infection develops, you should immediately contact your doctor about the further use of the bottle. If the application of drops is difficult after the first opening of the bottle, place the cap back on the bottle and tighten the cap (not very tightly), then unscrew the cap, turning it in the direction of the directional arrows on the top surface of the cap. 7. Repeat steps 4 and 5 for the other eye, if the drug should be instilled into both eyes. Close the bottle cap, twisting it until tight contact with the bottle. To properly close the arrow on the cap of the bottle must match the arrow on the label of the bottle. Do not over tighten the cap, otherwise the bottle or cap could be damaged. 9. Do not enlarge the opening of a specially designed dispensing tip.
Side effects
In clinical studies, Trusopt was prescribed to 1108 patients as monotherapy or additional therapy for treatment with beta-blockers. In approximately 3% of patients, the drug was canceled due to local adverse reactions from the side of the eye, the most frequent of which were conjunctivitis and eyelid reactions.The side effects registered during the research and during the post-registration period are classified by frequency: very frequent (> 1/10), frequent (≥1 / 100, <1/10); infrequent (≥1 / 1000, <1/100); rare (≥1 / 10000, <1/1000). From the nervous system: often - headache; rarely - dizziness, paresthesia. On the part of the organ of vision: very often - burning and pain; often - superficial point keratitis, lacrimation, conjunctivitis, inflammation of the eyelids, itching, irritation of the century, blurred vision; infrequently - iridocyclitis; rarely - redness of the eye, pain, hyperkeratosis of the eyelids, transient myopia (disappearing after drug withdrawal), corneal edema, reduction of intraocular pressure, detachment of the choroidal membrane of the eye after surgical interventions to restore the outflow of intraocular fluid. From the digestive system: often - nausea, bitter taste in the mouth; rarely - dry mouth. From the skin and mucous membranes: rarely - contact dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. From the urinary tract: rarely - urolithiasis. Allergic reactions: rarely - signs and symptoms of local reactions (from the ) and systemic allergic reactions, including angioedema, urticaria, pruritus, rash, difficulty breathing, less often - bronchospasm. On the whole body: often asthenia, fatigue. Children during a 3-month double-blind multicenter study I using the active drug as a control, conducted with 184 children under the age of 6 years, the side effect profile of the drug Trusopt was comparable to the side effect profile in adult patients. The most frequent adverse reactions associated with the use of the drug Trusopt in children under the age of 2 years were conjunctival injection (5.4%) and discharge from the eyes (3.6%). In children from 2 to 6 years old, the most frequent adverse reactions were burning sensation in the eye (12.1%), conjunctival injection (7.6%), eye pain (3%), inflammation of the eyelids (3%).
Overdose
Symptoms: possible electrolyte disturbances, the development of metabolic acidosis and the occurrence of drowsiness, nausea, dizziness, headache, weakness, unusual dreams, dysphagia.Treatment: plasma electrolyte concentrations (especially potassium) and blood pH should be monitored. In case of overdose, symptomatic therapy is carried out aimed at maintaining the vital functions of the body.
Interaction with other drugs
Special studies on the interaction of the drug Trusopt with other drugs have been conducted. In clinical studies, Trusopt was prescribed in combination with other drugs without negative manifestations of drug-drug interaction, including with eye drops of timolol and betaxolol, as well as systemic drugs: ACE inhibitors, calcium channel blockers, diuretics, NSAIDs (including acetylsalicylic acid), hormones (estrogen, insulin, thyroxine). It is not possible to enhance the systemic effects of carbonic anhydrase inhibitors for internal use and Trusopt drug with their simultaneous use. Combined treatment with drugs that have a systemic effect and local carbonic anhydrase inhibitors (Trusopt) has not been studied in clinical studies. The drug Trusopt is a carbonic anhydrase inhibitor, and although it is applied topically, it is partially absorbed and can have a systemic effect. In clinical studies, the use of the drug Trusopt was not accompanied by a violation of the acid-base balance. However, similar phenomena were observed when using carbonic anhydrase inhibitors, including and as a result of drug interactions with other drugs (as a manifestation of toxicity in patients receiving high doses of salicylates). Thus, when prescribing Trusopt, one should not forget about the possibility of such a drug interaction. The patient should inform the doctor about all the drugs that he uses or plans to use, including those that are sold without a prescription. Special attention should be paid to taking acetylsalicylic acid in high doses
special instructions
Patients who wear contact lenses should consult a physician before using Trusopt because a preservative in the product may cause eye irritation.The drug Trusopt contains benzalkonium chloride as a preservative, which can be adsorbed by contact lenses. Before using the drug lens must be removed; Do not wear lenses earlier than 15 minutes after instillation of the drug. Benzalkonium chloride can discolor soft eye lenses. Effect on the ability to drive vehicles and control mechanisms. During the period of treatment with Cruzopt, it is necessary to refrain from driving vehicles and practicing potentially hazardous activities that require increased concentration and psychomotor reactions.